Abstract: The invention provides a novel class of therapeutic agents that are safe and effective TYK2 inhibitors and pharmaceutical compositions of these compounds and methods of preparation and use thereof against various TYK2-mediated diseases and disorders.

Abstract: The invention described here provides ready-to-use (RTU) pharmaceutical compositions in single unit dose packaging, such compositions including ascorbic acid compound(s), such as sodium ascorbate, and one or more pharmaceutically acceptable excipients (e.g., a carrier and optionally other agents, such as a tonicity agent, a chelator, or both). The compositions provided by the invention are stable when stored at 20° C. to 25° C.±2° C. for at least about 3 months. Compositions provided by the invention comprise an osmolality of between about 270 mOsm/kg to about 340 mOsm/kg and do not require dilution or further manipulation prior to use. In certain aspects, the invention comprises methods of using such compositions in the treatment of diseases, conditions, or symptoms related to vitamin C deficiency, such as, in specific embodiments, scurvy.

Abstract: The disclosure provides processes for synthesizing Compound I, and pharmaceutically acceptable salts thereof.

Abstract: This patent document discloses novel compounds and methods of preventing or treating diseases or conditions related to Keap1-Nrf2 interaction activity by use of the novel compounds. As direct inhibitors of Keap1-Nrf2 interaction, the compounds disclosed herein are more specific and free of various undesirable effects than existing indirect inhibitors, and are potential dmg candidates of chemopreventive and therapeutic agents for treatment of various diseases or conditions involving oxidative stress and/or inflammation, including but not limited to cancers, diabetes, Alzheimer's, Parkinson's, and inflammatory bowel disease including ulcerative colitis.

Abstract: Disclosed are pharmaceutical compositions comprising a lyophilized compound of formula (I): (I) or a pharmaceutically acceptable salt thereof, and methods of using the same for treating cancer.

Abstract: The disclosure provides at least one entity chosen from compounds of Formula (I) pharmaceutically acceptable salts thereof, solvates of any of the foregoing, and deuterated derivatives of any of the foregoing, compositions comprising the same, and methods of using the same, including use in treating APOL1 mediated kidney disease.

Abstract: The invention provides fused heterocyclic organic compounds such as dihydropyrazolopyridotriazinones, compositions containing such compounds, medical kits, and methods for using such compounds and compositions for body contouring and/or reduction of fat in a subject.

Abstract: The present disclosures are directed to processes for synthesizing (S)-2-(((S)-6,8-difluoro-1,2,3,4-tetrahydronaphthalen-2-yl)amino)-N-(1-(2-methyl-1-(neopentylamino)propan-2-yl)-1H-imidazol-4-yl)pentanamide (“nirogacestat”).

Abstract: Embodiments of the present disclosure provide an injectable photothermal hydrogel based on melanin and a preparation method and an application thereof. The injectable photothermal hydrogel is a hydroxypropyl chitosan/bis-amino polyethylene glycol modified melanin nanoparticles (HPCS/MP) hydrogel. The HPCS/MP hydrogel is prepared by mixing bis-amino polyethylene glycol modified melanin nanoparticles (MP) with hydroxypropyl chitosan (HPCS). The MP is synthesized by an amidation reaction of the melanin and the bis-amino PEG. A ratio of a volume of an MP solution to a volume of an HPCS solution in the HPCS/MP hydrogel is 4:6. A concentration of the MP solution is 20 wt %. A concentration of the HPCS solution is 4 wt %.

Abstract: Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.

Abstract: A method for preparing dihydroartemisinin bulk drug in single process comprises: S1. dissolving artemisinin in aprotic solvent; S2. adding phase transfer catalyst and reducing agent in sequence to cause a reduction reaction with artemisinin; S3. adjusting the pH of the reaction system obtained in step S2 to 5-7 with acid solution, adding water and stirring, separating the liquids, extracting the aqueous phase obtained by the separation with the same aprotic solvent as in step S1, combining the organic phase obtained by extraction and separation, washing with water, and drying, obtaining dried organic phase; S4. placing the dried organic phase obtained in step S3 in a crystallization device that has the functions of crystallization-press filtration-drying, and then the crystals are precipitated, concentrated, press-filtered, and dried to obtain the refined dihydroartemisinin.

Abstract: A heterobifunctional monodispersed polyethylene glycol represented by the formula (1): wherein X1 and Y1 are each an atomic group containing a functional group capable of forming a covalent bond upon a reaction with a functional group present in a biofunctional molecule, the functional group contained in the atomic group X1 and the functional group contained in the atomic group Y1 are different from each other; R1 is a hydrocarbon group having from 1 to 7 carbon atoms or a hydrogen atom; n is an integer of 3 to 72; 1 is an integer of 2 to 72; and A1, B1 and C1 are as defined herein.

Abstract: The present disclosure relates to solid state forms of Reproxalap salts, processes for the preparation thereof, pharmaceutical formulations/compositions thereof, and methods of use thereof.

Abstract: In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

Abstract: The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR enzyme and are useful in the treatment of FGFR-associated diseases such as cancer.

Abstract: Disclosed herein are inhibitors of the GGDPS enzyme, and methods for their use in treating or preventing diseases, such as multiple myeloma. The inhibitors described herein can include compounds of Formula (I) and pharmaceutically acceptable salts thereof: wherein the substituents are described.

Abstract: A process is provided, comprising reacting a (hetero)aryl 1,3-dipole compound with a (hetero)cycloalkyne, wherein the (hetero)aryl 1,3-dipole compound comprises a 1,3-dipole functional group bonded to a (hetero)aryl group, and wherein the (hetero)aryl 1,3-dipole compound is a (hetero)aryl azide or a (hetero)aryl diazo compound; wherein: (i) the (hetero)aryl group of the (hetero)aryl 1,3-dipole compound comprises a substituent (ii) the (hetero)aryl group of the (hetero)aryl 1,3-dipole compound is an electron-poor (hetero)aryl group and wherein the (hetero)cycloalkyne is a (hetero)cyclooctyne or a (hetero)cyclononyne according to Formula (1). The invention also relates to the products obtainable by the process according to the invention.

Abstract: The present invention provides a heterocyclic compound having a HDAC inhibitory action, which is useful for the treatment of central nervous system diseases including neurodegenerative diseases, and the like, and a medicament comprising the compound. The present invention relates to a compound represented by the formula (I): wherein each symbol is as described in the description, or a salt thereof.

Abstract: Provided herein is an inositol polyphosphate oligo alkyl ether compound, or its pharmaceutically acceptable salt, for use in treatment or prevention of a disease associated with formation of calcium salt crystals.

Abstract: The specification relates to compounds of Formula (I): and to pharmaceutically acceptable salts thereof, to processes and intermediates used for their preparation, to pharmaceutical compositions containing them and to their use in the treatment of cell proliferative disorders.